imidazo[1,2-a]pyrimidin-6-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并[1，2-a]嘧啶
• 英文名称: imidazo[1,2-a]pyrimidin-6-amine
• 化学式: C₆H₆N₄
• mdl: MFCD10574905
• 分子量: 134.14
• InChiKey: BJZJBQBKRGDTPE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  56.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  imidazo[1,2-a]pyrimidin-6-amine 在 吡啶 作用下， 以 四氢呋喃 为溶剂， 反应 16.5h， 生成 (S)-1-(1-(5-fluoro-3-methylbenzofuran-2-yl)-2-methylpropyl)-3-(imidazo[1,2-a]pyrimidin-6-yl)urea
  参考文献：
  名称：

  [EN] UREA DERIVATIVES WHICH CAN BE USED TO TREAT CANCER
  [FR] DÉRIVÉS D'URÉE POUVANT ÊTRE UTILISÉS POUR TRAITER LE CANCER

  摘要：

  This disclosure provides compounds of Formula (I), Formula (II), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Ka). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3Ka activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

  公开号：

  WO2022265993A1

文献信息

• [EN] COMPOUNDS<br/>[FR] COMPOSÉS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2021239885A1

  公开（公告）日：2021-12-02

  The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.

  本发明涉及用于抑制NLRP3炎症体产生的新化合物，其中所述化合物由公式（I）定义，其中整数R1、R2和R3在描述中定义，且所述化合物可用作药物，例如用于治疗与NLRP3炎症体活性相关的一种疾病或失调。
• THERAPEUTIC AGENT FOR TAUOPATHIES
  申请人：Sumitomo Pharma Co., Ltd.

  公开号：EP4104861A1

  公开（公告）日：2022-12-21

  The present invention is to provide a medicament for treating and/or preventing tauopathy by activating the voltage-gated sodium channel (Nav). The present invention relates to a medicament for treating and/or preventing tauopathy, comprising a Nav activator as an active ingredient.

  本发明提供了一种通过激活电压门控钠通道（Nav）治疗和/或预防tau病的药物。本发明涉及一种治疗和/或预防tau病的药物，其包括Nav激活剂作为活性成分。
• [EN] NAMPT INHBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE NAMPT ET LEURS UTILISATIONS
  申请人：REMEDY PLAN INC

  公开号：WO2022241257A1

  公开（公告）日：2022-11-17

  Disclosed are compounds, methods, compositions, uses, and kits that modulate (e.g., inhibit) nicotinamide phosphoribosyltransferase (NAMPT), the production of nicotinamide mononucleotide (NMN), the production of nicotinamide adenine dinucleotide (NAD), NAMPT signaling, a NAMPT pathway, and/or cellular metabolism. In some embodiments, the compounds are used to treat diseases or disorders. The compounds may treat cancer by targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, lymphoma, liver cancer, endometrial cancer, leukemia, or multiple myeloma. Further provided are methods of manufacturing compounds of Formula (V). The compounds of the disclosure are of Formula (I), (II), (III), and (IV):

  本发明涉及调节（例如抑制）烟酰胺磷酸核糖转移酶（NAMPT）、烟酰胺单核苷酸（NMN）的产生、烟酰胺腺嘌呤二核苷酸（NAD）的产生、NAMPT信号传导、NAMPT途径和/或细胞代谢的化合物、方法、组合物、用途和试剂盒。在某些实施例中，这些化合物用于治疗疾病或疾病障碍。这些化合物可以通过靶向癌症干细胞来治疗癌症。在某些实施例中，这种癌症是结肠癌、胃癌、胃肠间质瘤、卵巢癌、肺癌、乳腺癌、胰腺癌、前列腺癌、睾丸癌、淋巴瘤、肝癌、子宫内膜癌、白血病或多发性骨髓瘤。此外，还提供了制造化合物公式（V）的方法。本公开的化合物为公式（I）、（II）、（III）和（IV）的化合物。
• ORGANIC LIGHT-EMITTING DEVICE
  申请人：Samsung Display Co., Ltd.

  公开号：EP3185325A1

  公开（公告）日：2017-06-28

  According to one or more embodiments, an organic light-emitting device comprises: a first electrode; a second electrode facing the first electrode; an emission layer between the first electrode and the second electrode; a hole transport region between the first electrode and the emission layer; and an electron transport region between the emission layer and the second electrode. The emission layer comprises a first compound represented by Formula 1, and at least one selected from the hole transport region and the electron transport region comprises a second compound represented by Formula 2A or 2B:

  根据一个或多个实施例，有机发光器件包括：第一电极；面向第一电极的第二电极；位于第一电极和第二电极之间的发射层；位于第一电极和发射层之间的空穴传输区域；以及位于发射层和第二电极之间的电子传输区域。发射层包括由式 1 表示的第一种化合物，空穴传输区和电子传输区中的至少一种由式 2A 或 2B 表示的第二种化合物组成：
• [1]BENZOTHIENO[3',2':4,5]IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN ORGANIC LIGHT-EMITTING DEVICES (OLEDS)
  申请人：Samsung Display Co., Ltd.

  公开号：EP3301097B1

  公开（公告）日：2020-08-19